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09/25/08 - USPTO Class 548 |  47 views | #20080234492 | Prev - Next | About this Page  548 rss/xml feed  monitor keywords

Process for the preparation of carvedilol

USPTO Application #: 20080234492
Title: Process for the preparation of carvedilol
Abstract: A process for the preparation of carvedilol of formula (I) (I) either in enantiomeric substantially pure form, or as an enantiomeric mixture, optionally as a pharmaceutically acceptable salt thereof, which process comprises reacting 2,3-eopxypropoxy carbazole of formula (II) (II) or the R or S enantiomer thereof, with N-[2-(2-methoxy-phenoxy)ethyl]-benzylamine of formula (V) (V) to yield benzyl carvedilol of formula (VI) (VI) which is debenzylated by catalytic hydrogenation to yield carvedilol of formula (I), either in enantiomeric substantially pure form, or as an enantiomeric mixture, and if desired reacting the thus formed carvedilol of formula (I) with an inorganic or organic acid to yield a pharmaceutically acceptable salt thereof, and/or, if desired, separating the enantiomers. The above process is characterised in that reaction of said 2,3-epoxypropoxy carbazole of formula (II) with said N-[2-(2-methoxy-phenoxy)ethyl]-benzylamine of formula (V) is carried out in water as the reaction medium. The present invention further provides carvedilol of formula (I) prepared by a process as described above, and pharmaceutical compositions containing the same and therapeutic uses thereof. (end of abstract)



USPTO Applicaton #: 20080234492 - Class: 548444 (USPTO)

Process for the preparation of carvedilol description/claims


The Patent Description & Claims data below is from USPTO Patent Application 20080234492, Process for the preparation of carvedilol.

Brief Patent Description - Full Patent Description - Patent Application Claims
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The present invention is concerned with a new process for preparing 1-(9H-carbazol-4-yloxy)-3-[[2-(2-methoxyphenoxy)ethyl]amino]-2-propanol of formula (I)

The above compound of formula (I) is known under the INN name of carvedilol and is used as a drug having antihypertensive, beta-adrenergic blocking and vasodilating activity.

The preparation of carvedilol has been known from DE 2815926, while the preparation of the R and S enantiomers has been described in DE 3313027. More particularly, 2,3-epoxypropoxy carbazole of formula (II)

or the R or S enantiomer thereof, is reacted with 2-[2′-(methoxy)-phenoxy]-ethylamine of formula (III)

to produce carvedilol in a yield of 39 to 42%. A drawback of this known process is that in addition to the formation of carvedilol, the following bis compound of formula (IV) is also formed

Further processes for the preparation of carvedilol have also been described in DE 2815926. In Example 5 of DE 2815926, 2,3-epoxypropoxy carbazole of above formula (II) is reacted with the secondary amine N-[2-(2-methoxy-phenoxy)ethyl]-benzylamine of formula (V)



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Patent Applications in related categories:

20090286991 - Process for the preparation of carvedilol form ii - A cost-effective, industrially feasible process for the manufacture of crystalline Carvedilol Form-II using novel Carvedilol salts comprises the steps of reacting 4-(2,3-epoxy propoxy)carbazole (II) with 2-(2-methoxy phenoxy)ethyl amine (III) followed by acidification with mineral acid in presence of an organic solvent to yield acid addition salts, treatment of the said ...


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